Ketoconazole in Advanced Prostate Cancer: Have Tolerability Concerns Been Overstated?

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Originally introduced into clinical practice over 20 years ago, ketoconazole† is a broad-spectrum imidazole antifungal agent that inhibits 14alpha-demethylase and thereby interrupts the synthesis of an essential fungal membrane sterol. As ketoconazole became widely used as an anti-fungal agent, it was noticed that a small number of male patients developed painful gynaecomastia; this led to the discovery of the inhibitory effects of the drug on gonadal and adrenal steroidogenesis. Ketoconazole has been shown to be a useful second-line treatment in patients with advanced prostate cancer, but its use has been limited by concerns over its adverse effects (notably those on the liver). Recent re-evaluation of the literature has suggested, however, that these concerns have been overstated and that the most serious potential adverse effects of ketoconazole can be avoided in the majority of patients.


† Ketoconazole is available in Spain, but is not approved for the treatment of advanced prostate cancer.



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